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CAS No.: 2101626-26-8

HPGDS inhibitor 2 Catalog No. CSN24192

Synonyms: GSK-2894631A;GSK-2894631

GSK-2894631A is a highly potent and selective HPGDS inhibitor with IC50 value of 9.9nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述H-PGDS (hematopoietic prostaglandin D synthase) is a member of the σ-class of glutathione-S-transferases, expressed in dendritic cells and Langerhans cells of skin, Kupffer cells in the liver, dendritic cells in the thymus, microglia in the brain, the oviduct, and megakaryocytes in the bone marrow, as well as in mast cells, eosinophils, and activated T_h2 cells in many tissues. It has been implicated in asthma, allergic rhinitis, Krabbe disease, Duchenne muscular dystrophy and lupus. GSK-2894631A is a selective and potent H-PGDS inhibitor with IC50 value of 9.9nM. It exhibited good murine pharmacokinetics, dose-dependently attenuated PGD2 production in a mast cell degranulation assay. GSK-2894631A attenuated PGD2 release to baseline levels in a dose-dependent manner with an ED50 of 0.032mg/kg a murine mast cell degranulation model of inflammation orally dosed of GSK-2894631A at 0.03mg/kg to 3mg/kg^[2].
作用机制GSK-2894631A binds to the ligand binding site of hH-PGDS.^[2]

动物研究

剂量

Mice: 0.03 mg/kg - 3 mg/kg^[1] (p.o.)

给药途径

p.o.

动物药代数据

Animal	Mice^[1]
Dose	0.03 mg/kg - 3 mg/kg
Administration	p.o.
F	0.61
P_app	240 nm/s
T_1/2	3.8 h
CL	5.6 ml/min/kg
FaS-SIF	0.070 mg/ml
Vss	1.7 L/kg
DNAUC	1800 ng/h/ml

参考文献

[1] Deaton DN, Do Y, et al. The discovery of quinoline-3-carboxamides as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors. Bioorg Med Chem. 2019 Apr 15;27(8):1456-1478.
[2] Deaton DN, Do Y, Holt J, Jeune MR, Kramer HF, Larkin AL, Orband-Miller LA, Peckham GE, Poole C, Price DJ, Schaller LT, Shen Y, Shewchuk LM, Stewart EL, Stuart JD, Thomson SA, Ward P, Wilson JW, Xu T, Guss JH, Musetti C, Rendina AR, Affleck K, Anders D, Hancock AP, Hobbs H, Hodgson ST, Hutchinson J, Leveridge MV, Nicholls H, Smith IED, Somers DO, Sneddon HF, Uddin S, Cleasby A, Mortenson PN, Richardson C, Saxty G. The discovery of quinoline-3-carboxamides as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors. Bioorg Med Chem. 2019 Apr 15;27(8):1456-1478. doi: 10.1016/j.bmc.2019.02.017. Epub 2019 Feb 11. PMID: 30858025.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6426 mL
- 13.2131 mL
- 26.4262 mL
- 5 mM
- 0.5285 mL
- 2.6426 mL
- 5.2852 mL
- 10 mM
- 0.2643 mL
- 1.3213 mL
- 2.6426 mL

技术信息

CAS号

2101626-26-8

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H24F2N2O3

运输

蓝冰

分子量

378.41

别名

GSK-2894631A;GSK-2894631

溶解度

DMSO	150.0 mg/mL (396.4 mM)

动物实验配方

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